衍生化毛细管气相色谱法测定人尿液中甘露醇和乳果糖

目的建立毛细管气相色谱法测定人尿液中甘露醇和乳果糖含量.方法用衍生化毛细管气相色谱法,以对照品为外标,色谱柱为SE-30石英毛细管柱(25mm×0.22mmID);柱温起始温度200℃,以15℃*min-1升温至300℃维持10min;进样温度220℃;检测器温度300℃.结果甘露醇和乳果糖的线性范围均在1.25～5.0mg*ml-1范围内,相关系数分别为0.9970和0.9945,平均回收率分别为99.25%和99.34%,RSD为1.02%和0.61%.结论方法灵敏、准确、重现性好,可用于测定生物液体中甘露醇和双糖.     

毛细管色谱法测定替莫唑胺酯中的有机溶剂残留量

目的建立毛细管气相色谱法测定替莫唑胺酯中的有机溶剂残留量。方法采用INNOWax毛细管气相色谱柱、FID检测器,以乙腈为内标进行测定。结果正己醇、丙酮、乙酸乙酯、异丙醇、正己烷、吡啶的线性范围分别为25～400μg.L-1(r=0.999 6)、25～400μg.L-1(r=0.999 9)、25～400μg.L-1(r=0.999 9)、25～400μg.L-1(r=0.999 7)、1.45～23.2μg.L-1(r=0.999 8)和1～16μg.L-1(r=0.999 3);正己醇、丙酮、乙酸乙酯、异丙醇、正己烷、吡啶的平均回收率分别为99.7%、100.3%、100.2%、100.4%、99.9%和100.3%;RSD分别为1.11%、1.43%、1.47%、1.37%、1.59%和1.47%(n=9)。结论该方法简单、灵敏、准确、重现性好,适用于替莫唑胺酯中的有机溶剂残留量的测定。     

胶束电动色谱法同时测定冬凌草片中冬凌草甲、乙素的含量

目的:建立同时测定冬凌草片中冬凌草甲、乙素含量的方法。方法:采用胶束电动色谱法。运行溶液为25mmol.L-1的十二烷基硫酸钠(SDS)Tris缓冲液,电压25kV,检测波长为240nm。结果:冬凌草甲、乙素的线性范围分别为50~300mg.L-1、25~200mg.L-1,平均回收率分别为99.7%,99.6%。结论:该方法准确可靠、方便快捷,能有效地控制药品质量。     

HPLC测定氟康唑莫西沙星眼用即型凝胶的含量

目的建立高效液相色谱法测定氟康唑莫西沙星眼用即型凝胶含量,同时测定制剂中氟康唑、莫西沙星和羟苯乙酯的含量。方法采用ODS-C18色谱柱,以三乙胺缓冲液-甲醇为流动相,流速1.0 mL.min 1,检测波长260 nm。结果氟康唑、莫西沙星、羟苯乙酯的线性范围分别为25～250 g.mL 1(r=0.999 9,n=6),25～250 g.mL 1(r=0.999 9,n=6),2.5～25 g.mL 1(r=0.999 7,n=6),平均回收率分别为99.6%,99.4%,99.3%。RSD分别为1.23%,1.20%,1.17%。结论本方法操作简便,灵敏度高,重复性好,可用于该制剂的含量测定。     

HPLC法测定左金胶囊中4种生物碱的含量

目的：建立测定左金胶囊中4种生物碱含量的方法。方法：色谱柱为ODS柱（250 mm×4.6 mm,5μm）;流动相为乙腈-0.05 mo.lL-1磷酸二氢钾溶液（52∶48,含25 mmol.L-1十二烷基磺酸钠,磷酸调至pH3.0）;流速为1 mL.min-1;柱温为25℃;检测波长为225 nm,进样量为20μL。结果：盐酸小檗碱、盐酸巴马汀、吴茱萸碱和吴茱萸次碱的线性范围分别为12.18～121.8、3.016～30.16、0.081 55～0.815 5和0.042 96～0.429 6 mg.L-1,相关系数分别为0.9997、0.999 4、0.998 6和0.997 4;平均回收率分别为99.25%、101.80%、97.56%和96.19%,RSD分别为1.45%、1.39%、1.72%和1.87%（n=5）。结论：该法灵敏度高、重复性好,可用于左金制剂的质量控制。     

司帕沙星治疗非淋菌性泌尿生殖道炎30例

目的:评价司帕沙星治疗非淋菌性泌尿生殖道炎的疗效及安全性.方法:患者 60例,其中口服司帕沙星组 (治疗组 )30例, 200～ 300 mg/次, 1次 /d;口服阿奇霉素组 (对照组 )30例, 250～ 1 000 mg/次, 1次 /d.疗程均为 7～ 14 d.结果:治疗组和对照组有效率分别为 90. 0%和 86.7%,痊愈率分别为 83.3%和 80.0%,病原菌清除率分别为 90.0%和 86.7%,不良反应发生率为 3.33%和 6.67%.经统计学处理无显著差异 (P > 0.05).结论:司帕沙星治疗非淋菌性泌尿生殖道炎安全、有效.     

HPLC梯度洗脱法测定舒胸片中羟基红花黄色素A和阿魏酸的含量

目的：建立舒胸片（三七、川芎、红花）中羟基红花黄色素A、阿魏酸的含量HPLC测定方法.方法：用Agilent ODSC18柱（250 mm×4.6 mm,5 μm）,流动相为甲醇0.12%磷酸溶液,梯度洗脱（0～17 min,25%甲醇;17～30 min,25%～40%甲醇）;流速1 ml·min-1;波长分别为403 nm和320 nm;柱温35℃.结果：羟基红花黄色素A、阿魏酸得到很好分离,线性关系良好,羟基红花黄色素A、阿魏酸的平均加样回收率分别为100.0%,99.6%,RSD分别为1.19%,1.33%（n=5）.结论：本法结果准确,便于操作,可作为舒胸片的质量控制方法之一.     

贝沙罗汀软胶囊在复发难治性皮肤T细胞淋巴瘤患者中的药代动力学研究

目的:评价贝沙罗汀在复发难治性皮肤T细胞淋巴瘤患者中的药物代谢动力学。方法:建立荧光液相色谱法,以乙腈、乙酸铵、乙酸等为流动相成分,在激发波长260 nm、发射波长430 nm的色谱条件下进行方法学考察及血药浓度测定。所得到的血药浓度以DAS 2.0药代动力学参数计算程序进行参数计算。皮肤T细胞淋巴瘤患者接受贝沙罗汀口服300 mg.m-2,qd,连用4周,进行单剂量和多剂量药代动力学分析。结果:建立的荧光液相色谱法在10～1 000 ng.mL-1之间线性关系良好(r=0.999 7),在空白血浆中20,100和800 ng.mL-1浓度的提取回收率分别为79.49%8,7.06%和78.56%。血药浓度测定结果显示,5例皮肤T-细胞淋巴瘤患者口服贝沙罗汀软胶囊300 mg.m-2,服药d 1和连续服药d 28的Cmax分别为366.31和652.44 ng.mL-1;Tmax分别为1.80和1.88 h;t1/2分别为2.56和3.18 h;AUC0～t分别为1 680.96和2 133.34ng.mL-1.h。结论:建立的荧光液相色谱法稳定,敏感性高。皮肤T-细胞淋巴瘤患者口服300 mg.m-2的贝沙...     

HPLC法同时测定复方黄芪注射液中人参皂苷Re、Rg_1含量

目的建立HPLC法同时测定复方黄芪注射液中人参皂苷Re、Rg1的含量。方法采用HPLC法,色谱柱为DiamonsilTM C18柱(4.6 mm×250 mm,5μm),流动相为乙腈50 mmol.L-1磷酸二氢钾缓冲溶液(体积比为20∶80),柱温为25℃,检测波长为203 nm,流速为1.0 mL.min-1。结果复方黄芪注射液中人参皂苷Re、Rg1与其他成分分离良好。人参皂苷Re的质量浓度在25~500 mg.L-1内(r=0.999 8)、Rg1的质量浓度在25~300 mg.L-1(r=0.999 8)内与峰面积线性关系良好,人参皂苷Re、Rg1的回收率分别为100.2%和99.8%,RSD分别为1.4%和2.0%。结论方法准确、重现性好,可用于复方黄芪注射液的质量控制。     

司帕沙星治疗女性非淋菌性泌尿生殖道感染27例

目的:评价司帕沙星治疗女性非淋菌性泌尿生殖道感染的临床疗效.方法:将55例患者随机分为两组.治疗组27例,口服司帕沙星200～300 mg,1次/d;对照组28例,口服阿奇霉素250 mg,1次/12 h.疗程7～14 d.结果:司帕沙星组与阿奇霉素组有效率分别为88.9%和92.9%,痊愈率分别为85.2%和82.1%,病原菌清除率分别为92.6%和92.9%,不良反应发生率分别为3.7%和7.1%,两组疗效无显著性差异(P＞0.05).结论:司帕沙星与阿奇霉素治疗女性非淋菌性泌尿生殖道感染的疗效和安全性相似.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.